Morphinans are important pharmaceuticals that typically are used as analgesics or drug/alcohol cessation agents. Substituted morphinans, such as 6-amino derivatives, may be useful therapeutically because they have higher efficacy, greater potency, and/or may function as prodrugs. Moreover, the potency of particular morphinan compounds may be increased by particular configurations at the chiral centers of the compounds. Although several methods for forming 6-amino morphinans from 6-keto morphinans have been reported in the literature, none provides the selective synthesis of 6-amino morphinans, wherein the morphinan compounds lack the 4,5-epoxy ring, which produces particular epimers and diastereomers in good yield. There is a need, therefore, for simple, mild, and efficient processes for the preparation of these diastereomerically or epimerically enriched 6-amino morphinans.